Astellas aims to create a continuous stream of innovative medicines. We focus on steady progress of six key late stage projects so that we can deliver the value to patients as soon as possible.

Please see here for the details of target diseases and status for each project.
 

 

enzalutamide (brand name: XTANDI)

Enzalutamide is marketed worldwide for the treatment of castration-resistant prostate cancer (CRPC). As an additional indication, it was approved also for the treatment of metastatic castration-sensitive prostate cancer (M1 CSPC) in the US and for the treatment of prostate cancer patients with distant metastasis in Japan. Astellas is developing to expand the indications to earlier stages of prostate cancer in collaboration with Pfizer, Inc.

Enzalutamide is an androgen receptor (AR) inhibitor. It targets the AR and exerts its effects on three steps of the AR signaling pathway: inhibiting androgen binding to the receptor; preventing nuclear translocation; impairing DNA binding of the AR to the DNA.

Prostate cancer is the second most common in the cancers in men, and annually 1.3 billion men is newly diagnosed worldwide.*1 Astellas focuses on the further development so that enzalutamide can contribute to more patients.

*1 World Health Organization Cancer Fact Sheet 2018

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gilteritinib (brand name: XOSPATA)

Gilteritinib is marketed for the treatment of patients with relapsed or refractory FLT3 mutation-positive acute myeloid leukemia (AML) in Japan, the US, and the EU. Astellas is developing gilteritinib to expand the indications to earlier stages of AML.

Gilteritinib inhibits mutated FLT3, a receptor type tyrosine kinase known to be involved in cancer cell proliferation. FLT3 mutations are seen in approximately one-third of patients with AML.*1 Gilteritinib has demonstrated inhibitory activity against major type of mutations that are internal tandem duplication and tyrosine kinase domain.

AML is a cancer that is most commonly experienced in elderly people with the incidence rate increasing with age. The number of newly diagnosed AML patients are approximately 5,500 in Japan,*2 19,000 in the US*3 and 18,400 in the European Union*4 each year. AML is a life-threatening disease and requires early intervention. Induction and consolidation chemotherapy are the current standard care. However, resistance to current AML treatments and ineligibility of high-intensity induction chemotherapy for elderly patients due to an excessive physical burden make challenges in AML treatment. Promising new treatment options targeting specific genetic mutations have been awaited in AML treatment landscape.

*1 Patel JP, et al., 2012
*2 KantarHealth. TREATMENT ARCHITECTURE: JAPAN LEUKEMIA, ACUTE MYELOID. CancerMPact® Japan, February 2017
*3 American Cancer Society. Key Statistics for Acute Myeloid Leukemia (01-04-2018),
*4 Visser O, et al., 2012

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enfortumab vedotin (brand name: PADCEV)

Astellas is developing enfortumab vedotin as a treatment for urothelial cancer under collaboration with Seattle Genetics, Inc. In the US, enfortumab vedotin is marketed by Seattle Genetics, Inc. for the treatment of locally advanced or metastatic urothelial cancer, previously treated with platinum and anti-PD-1/PD-L1 antibody. Further development is ongoing to expand the regions and the indications to earlier stages of urothelial cancer.

Enfortumab vedotin is an investigational antibody drug conjugate (ADC)*1 composed of an anti-Nectin-4 monoclonal antibody attached to a microtubule-disrupting agent, MMAE, using Seattle Genetics’ proprietary linker technology. Enfortumab vedotin targets Nectin-4, a cell adhesion molecule that is expressed on many solid tumors.

Urothelial cancer is the most common type of bladder cancer (90 percent of cases). Globally, approximately 549,000 people were diagnosed with bladder cancer annually, and there are approximately 200,000 deaths worldwide.*2 It is known that Nection-4 is highly expressed in urothelial cancer.*3

Enfortumab vedotin is currently under development also in other solid tumors.

*1 Antibody drug conjugate (ADC): ADCs are monoclonal antibodies that are designed to selectively deliver cytotoxic agents to cancer cells.
*2 World Health Organization Cancer Fact Sheet 2018
*3 Challita-Eid PM, et al., 2016

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zolbetuximab

Astellas is developing zolbetuximab as a treatment for gastric and gastroesophageal junction (GEJ) cancer.

Zolbetuximab is an antibody that targets Claudin 18.2, a transmembrane protein that forms a tight junction connecting and binding two adjoining cell membranes. In normal cells, Claudin 18.2 is expressed locally in stomach cells, while it is expressed in various cancer types including gastrointestinal adenocarcinomas as well as pancreatic, biliary duct, ovarian and lung cancers.

Gastric and GEJ cancer is one of the malignancies with the highest unmet medical needs. Gastric cancer is the third leading cause of cancer death worldwide.*1 Moreover, the overall five-year survival rate for metastatic gastric and GEJ cancer is under 20%.*2 Chemotherapy and anti-HER2 antibodies are widely used for the treatment of metastatic or recurrent gastric and GEJ cancer. However, other therapeutic options are awaited especially in HER2-negative patients with a lack of effective targeted therapies.

Zolbetuximab is currently under development also in pancreatic adenocarcinoma. Pancreatic cancer is the seventh leading cause of cancer death worldwide,*1 and shows low overall five-year survival rate as 4%.*3

*1 World Health Organization Cancer Fact Sheet 2018.
*2 Pennathur A, et al., 2013; Sahin et al., 2008
*3 Ilic M, et al., 2016

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roxadustat (brand name: EVRENZO)

Astellas is developing roxadustat as a treatment for anemia associated with chronic kidney disease (CKD) on dialysis and not on dialysis, in collaboration with FibroGen Inc. Astellas has the development and commercialization rights in Japan, Europe, the Commonwealth of Independent States, the Middle East and South Africa. Roxadustat is marketed in Japan for the treatment of renal anemia on dialysis.

Roxadustat has a new mechanism of action, inhibiting hypoxia-inducible factor (HIF) prolyl hydroxylase (PH). By inhibiting HIF-PH, roxadustat increases HIF involved in the production of red blood cells, thereby enhancing the production of red blood cells and improving anemia.

Anemia is one of the common complications of CKD. It is reported that the progression of anemia in CKD leads to end-stage renal disease and increases the mortality rate.*1

Roxadustat can be administered orally and demonstrates equivalent efficacy and safety to the conventional treatments with erythropoietin-stimulating agent injections, as well as reducing the need for iron injections.*2,3 This is expected to be a new treatment option, which provides both effectiveness and convenience for patients.

Roxadustat is currently under development also in chemotherapy-induced anemia.

*1 Stauffer ME, et al., 2014
*2 American Society of Nephrology Kidney Week 2019
*3 European Renal Association-European Dialysis and Transplant Association 2020

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fezolinetant

Astellas is developing fezolinetant as a non-hormonal treatment for menopause-related vasomotor symptoms (MR-VMS: hot flashes and night sweats).

Fezolinetant is an antagonist of the NK3 receptor. Fezolinetant works by blocking neurokinin B (NKB) signaling and normalizing KNDy (kisspeptin/NKB/dynorphin) neuron activity, which modulates the temperature control center and reduces the frequency and severity of MR-VMS.

Hot flashes are the most common symptom for women transitioning through menopause.*1 Globally, approximately 57 percent of women aged 40 to 64 years have reported the occurrence of hot flashes and sweating.*2

VMS have a significant impact on women's quality of life (QoL), including sleep. Currently, there are limited non-hormonal options for managing it, and new safe and effective non-hormonal therapeutics are needed.

*1 Freedman RR, 2014
*2 Utian WH, 2005

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